Bill Chobotar (Biology), Desmond Murray (Chemistry), Karen Reiner (Medical Laboratory Science)
Synthesis and Biological Activity of Boronic Stilbenes
The purpose of this proposed collaborative, interdisciplinary (chemistry, biology, clinical laboratory sciences) research project is systematic development of novel boronic acid stilbenes as potential hybrid antibacterials and antiparasitic agents. This proposal is specifically based on: (a) independent research projects in organic synthesis of hybrid chalcones and stilbenes conducted by undergraduates under Dr. Desmond Murray's supervision, (b) a collaborative Master's thesis by Andrija Matak involving synthesis and antiparasitic activity of hybrid boronic chalcones supervised by Dr. Bill Chobotar and Dr. Desmond Murray and (c) antibacterial testing of hybrid chalcones and stilbenes by Clinical Laboratory Science seniors under Dr. Karen Reiner's guidance.
Each of these successful projects have clearly and cumulatively demonstrated promising results that this new project builds upon. Our proposed one-step synthesis will facilitate preparation (including purification) of multiple structural variations of boronic stilbenes and subsequent structure- activity (antibacterial and antiparasitic) studies. Research into the design, synthesis and biological activity of hybrid small molecules, possessing multiple pharmacophores and mechanisms of action, is a relatively new approach in drug development that seeks to increase potency while simultaneously decreasing emergence of resistance. In this context, our research into the biological activity of novel hybrid boronic stilbenes lies at the cutting edge of pharmaceutical research and development, while still being able to provide pedagogical instruction and research opportunities to both undergraduate and graduate students.
Specifically, this proposal seeks phase one funding for research supplies and materials and support for a biology graduate research assistant involved in a highly collaborative, interdisciplinary two-year, Master's thesis project.